2. Academic Validation
  3. Conjugates of betulin derivatives with AZT as potent anti-HIV agents

Conjugates of betulin derivatives with AZT as potent anti-HIV agents

  • Bioorg Med Chem. 2010 Sep 1;18(17):6451-69. doi: 10.1016/j.bmc.2010.06.092.
Juan Xiong 1,  Yoshiki Kashiwada,  Chin-Ho Chen,  Keduo Qian,  Susan L Morris-Natschke,  Kuo-Hsiung Lee,  Yoshihisa Takaishi
Affiliations

Affiliation

  • 1 Graduate School of Pharmaceutical Sciences, University of Tokushima, Tokushima 770-8505, Japan.
PMID: 20673723 DOI: 10.1016/j.bmc.2010.06.092
Abstract

Fourteen novel conjugates of 3,28-di-O-acylbetulins with AZT were prepared as anti-HIV agents, based on our previously reported potent anti-HIV triterpene leads, including 3-O-acyl and 3,28-di-O-acylbetulins. Nine of the conjugates (49-53, 55, 56, 59, and 60) exhibited potent anti-HIV activity at the submicromolar level, with EC(50) values ranging from 0.040 to 0.098muM in HIV-1(NL4-3) infected MT-4 cells. These compounds were equipotent or more potent than 3-O-(3',3'-dimethylsuccinyl)betulinic acid (2), which is currently in Phase IIb anti-AIDS clinical trial.

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